依鲁替尼纳米晶的制备工艺研究  

Preparation of Ibrutinib Nanocrystals

作　　者：周洁 刘云[1,2] 冯菊红[1,2] 汪诗雨[1,2] 葛燕丽[1,2] 胡学雷 ZHOU Jie;LIU Yun;FENG Juhong;WANG Shiyu;GE Yanli;HU Xuelei(School of Chemical Engineering and Pharmacy,Wuhan Institute of Technology,Wuhan 430205,China;Key Laboratory of Green Chemical Process of Ministry of Education,Wuhan 430205,China)

机构地区：[1]武汉工程大学化工与制药学院,湖北武汉430205 [2]绿色化工过程教育部重点实验室,湖北武汉430205

出　　处：《化学与生物工程》2024年第4期50-54,63,共6页Chemistry & Bioengineering

基　　金：湖北省自然科学基金重点项目(2011CDA048)。

摘　　要：为改善依鲁替尼(IBR)的水溶性和溶出度,采用湿法介质研磨法制备了依鲁替尼纳米晶(IBR-NC),采用单因素实验优化了IBR-NC的制备工艺,并通过粒径分析、扫描电镜(SEM)、X-射线粉末衍射(XRPD)分析、差示扫描量热(DSC)分析及溶出度实验对IBR-NC的质量进行了评价。结果表明,以PVP-K30-SDS为稳定剂,在物料比(IBR、PVP-K30、SDS的质量比)为10∶4∶1、IBR用量为120 mg、氧化锆珠规格为0.3 mm、氧化锆珠用量为40 g、研磨转速为150 r·min^(-1)、研磨时间为2.0 h的最优条件下,制备的IBR-NC的粒径为(224.7±5.7)nm、PDI为0.151±0.017,累积溶出率在10 min能达到99.49%,溶出效果良好,且放置90 d后依然具有良好的溶出性质。To improve the water solubility and dissolution of Ibrutinib(IBR),we prepared Ibrutinib nanocrystals(IBR-NC)by a wet media milling method.Moreover,we optimized the preparation process of IBR-NC by single-factor experiments,and evaluated the quality of IBR-NC by particle size analysis,scanning electron microscope(SEM)analysis,X-ray powder diffraction(XRPD)analysis,differential scanning calorimetry(DSC)analysis,and dissolution experiments.The results show that,the particle size and PDI of IBR-NC are(224.7±5.7)nm and 0.151±0.017,respectively,under the optimal conditions as follows:using PVP-K30-SDS as a stabilizer,the material ratio(mass ratio of IBR,PVP-K30,and SDS)of 10∶4∶1,the IBR amount of 120 mg,the zirconia bead diameter of 0.3 mm,the zirconia bead amount of 40 g,the grinding speed of 150 r·min^(-1),and the grinding time of 2.0 h.The prepared IBR-NC has good dissolution effect with the cumulative dissolution rate of 99.49%within 10 min,and still has good disslution properties after being placed for 90 d.

关 键 词：依鲁替尼 湿法介质研磨法 纳米晶 累积溶出率 

分 类 号：TQ463[化学工程—制药化工]